可樂定
Clonidine
Clonidine hydrochloride (imidazoline derivative)
別名: Duraclon · Jenloga · Catapres-TTS · ST-155 · clonidini hydrochloridum · Adesipress-TTS · Arkamin · Aruclonin · Atensina · Barclyd · Cantanidin · Caprysin · Catanidin · Catapresan · Catapressan · Clonistada · Clonnirit · Dispaclonidin · Dixarit · Epiclodina · Glausine · Haemiton · Menograine · Mirfat · Normopresan · Paracefan · Tenso-Timelets · Clonidina · Clonidine hydrochloride · Clonidinum
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
經審核的 v13 劑量證據
結構化劑量計算證據Adjunctive antidiarrheal therapy for refractory cases of inflammatory bowel disease (extra-label)
須由已驗證獸醫確認
- q8-12h
NA
必須一併考量的臨床脈絡 (2)
- ■ This medicine may be given with or without food. If your animal vomits or acts sick after receiving this medicine on an empty stomach, try giving the next dose with food or a small treat. If vomiting continues, contact your veterinarian.
- Clonidine tablets should be stored in tight, light-resistant containers at room temperature, 25°C (77°F); excursions from 15°C to 30°C (59°F-86°F) are permitted. The preservative-free injection for epidural use should be stored at controlled room temperature, 20°C to 25°C (68°F-77°F). Because it contains no preservative, unused portions of the injection should be discarded.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
可樂定是一種中樞 alpha-2 腎上腺素受體激動劑，在獸醫學中傳統上用作診斷犬隻生長激素 (GH) 缺乏症或嗜鉻細胞瘤的診斷劑。它也作為難治性炎症性腸病 (IBD)（特別是貓）的輔助治療，以及用於嚴重疼痛或手術麻醉的硬膜外輔助藥物。
臨床要點（藥理學補充）：
- 雖然藥典強調其診斷和胃腸道用途，但可樂定在現代獸醫行為醫學中越來越多地被標示外使用，以控制犬隻的恐懼性焦慮、噪音恐懼症和情境性恐慌。
- 它透過抑制交感神經喚醒來提供抗焦慮和鎮靜作用，通常不會出現其他鎮靜劑常見的嚴重共濟失調。
- 由於其心血管效應，需要仔細篩選病患並調整劑量。
作用機轉
Clonidine acts centrally at the brain stem, stimulating alpha-2 adrenoreceptors.
- Cardiovascular/Sympathetic: Stimulation of presynaptic alpha-2 receptors (e.g., in the locus coeruleus) → decreases norepinephrine release → reduces sympathetic outflow from the CNS → decreased peripheral resistance, heart rate, and blood pressure.
- Endocrine: Stimulates GHRH (Growth Hormone Releasing Hormone) → transient release of Growth Hormone (GH).
- Analgesia: Stimulates presynaptic and postjunctional alpha-2 adrenoreceptors in the dorsal horn of the spinal cord → blocks pain signal transmission to the brain.
- Gastrointestinal: Alpha-2 stimulation alters enteric nervous system tone, increasing fluid absorption and decreasing motility, aiding in refractory IBD.
安全性與警告
禁忌症
- Known hypersensitivity to clonidine
- Severe cardiovascular disease (use with extreme caution)
- Renal disease (use with extreme caution)
不良反應
- Transient hyperglycemia
- Dry mouth
- Constipation
- Aggressive behavior
- Hypotension
- Collapse
- Bradycardia
- Transient sedation
- Rebound hypertension (if withdrawn abruptly)
注意事項
Clonidine has a narrow margin of safety. It should be used with caution in patients with severe cardiovascular disease, including conduction disturbances or heart failure. Use very cautiously in patients with renal failure. Abrupt withdrawal, especially when used with beta-blockers, may cause rebound hypertension.
藥物交互作用
Possible additive hypotensive effects
May enhance bradycardia. If discontinuing, beta-blocker should be stopped first, then clonidine tapered to avoid rebound hypertension.
May exacerbate the actions of other CNS depressant drugs
Possible additive bradycardia
May decrease the antihypertensive effects of clonidine
May block the antihypertensive effects of clonidine
Increased central nervous system depression and hypotension
Additive sedation, bradycardia, and respiratory depression
Additive hypotensive and bradycardic effects; may exacerbate rebound hypertension upon withdrawal
Additive lowering of blood pressure
監測
- Growth Hormone (GH) levels and adverse effects (when used for diagnostics)
- Blood pressure
- Heart rate
- Efficacy and adverse effect profile (when used for ongoing diarrhea treatment)
- Degree of sedation
- Behavioral response
- Plasma IGF-1 or GH levels (when used diagnostically)
藥物動力學
半衰期
吸收
Well absorbed after oral administration in humans (peak plasma 3-5 hours). After epidural administration, maximal analgesia occurs within 30-60 minutes.
分佈
Widely distributed into body tissues; tissue concentrations are higher than in plasma. Enters the CSF, but brain concentrations are low compared with other tissues. In cats, exhibits a two-compartment open model and penetrates tissues rapidly.
代謝
Metabolized in the liver; one active metabolite (p-hydroxyclonidine) has been identified.
排除
Up to 60% of a dose is eliminated unchanged in the urine. Elimination may be prolonged with higher dosages (dose-dependent elimination kinetics) or in renal dysfunction.
過量
Clonidine has a narrow margin of safety.
- Clinical Signs: Hypotension, bradycardia, vomiting, weakness, depression, lethargy, tachycardia, ataxia, and hypertension. Rarely, seizures or respiratory depression.
- Toxicity Values: LD50 for oral clonidine in rats is 465 mg/kg; mice 206 mg/kg.
- Treatment: For large overdoses, gut evacuation using standard protocols (use emetics cautiously as consciousness may deteriorate rapidly). Symptomatic and supportive care. Fluids and pressors (e.g., dopamine) for hypotension. IV atropine for bradycardia. Atipamezole or yohimbine may be used to reverse cardiovascular effects, but multiple doses may be required as signs can last up to 48 hours.
可用產品
劑型
- Epidural injection
- Oral tablets
- Oral modified-release tablets
- Transdermal patch
- Injectable: 150 μg/ml solution
- Oral: 25 μg tablets
人用標示
- Clonidine HCl Injection for epidural use: 100 micrograms/mL & 500 micrograms/mL preservative-free (Duraclon)
- Clonidine HCl Oral Tablets: 0.1 mg, 0.2 mg & 0.3 mg (Catapres, generic)
- Clonidine HCl Oral Modified-release Tablets: 0.1 mg (Jenloga)
- Clonidine HCl Transdermal: 0.1 mg/24hrs, 0.2 mg/24hrs, & 0.3 mg/24hrs (Catapres-TTS-1, 2, or 3)
- Catapres 150 μg/ml injectable solution
- Catapres 25 μg oral tablets
各地核准狀態
POM (Prescription Only Medicine)
POM-V
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored in tight, light-resistant containers at room temperature (15-30°C / 59-86°F). Preservative-free injection for epidural use should be stored at controlled room temperature (25°C); unused portions must be discarded.
飼主須知
用途： 您的獸醫開立了可樂定來幫助控制您寵物的病情，這可能包括嚴重腹瀉、疼痛管理，或用於嚴重焦慮和恐懼症的標示外使用。
- 嚴格給藥： 可樂定的安全範圍很窄。請務必給予確切的處方劑量。切勿給予超過指示的劑量。
- 副作用： 注意是否有嚴重嗜睡、虛弱、牙齦蒼白或意外的行為改變（如攻擊性）的跡象。如果出現這些情況，請聯繫您的獸醫。
- 請勿突然停藥： 未經獸醫諮詢，請勿突然停止使用此藥物，因為這可能會導致血壓危險地飆升（反彈性高血壓）。
- 意外誤食： 請放置於所有寵物和兒童接觸不到的地方。如果發生過量服用，請立即尋求緊急獸醫護理。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。